Abstract
The diterpene, (-)- ent-kaur-16-en-19-oic acid, from Croton oblongifolius was identified as an Na +,K +-ATPase inhibitor. This compound exhibits an IC 50 of 2.2 x 10( -5 )M against crude enzyme Na +,K +-ATPase from rat brain. The semi-synthetic derivatives, (-)-methyl kaur-16-en-19-oate, (-)-kaur-16-en-19-ol, (-)-16beta,17-epoxykauran-19-oic acid and (-)-17-hydroxykaur-15-en-19-oic acid were also tested and their IC 50 were 5.5 x 10 (-4), 5.0 x 10( -4), 4.8 x 10( -4) and 6.0 x 10 (-4) M, respectively.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Brain / drug effects
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Brain / enzymology
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Croton*
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Diterpenes / administration & dosage
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Diterpenes / pharmacology*
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Diterpenes / therapeutic use
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / administration & dosage
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Enzyme Inhibitors / pharmacology*
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Enzyme Inhibitors / therapeutic use
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Inhibitory Concentration 50
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Phytotherapy*
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Plant Bark
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Plant Extracts / administration & dosage
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Plant Extracts / pharmacology
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Plant Extracts / therapeutic use
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Plant Stems
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Rats
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Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors*
Substances
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Diterpenes
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Enzyme Inhibitors
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Plant Extracts
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argyrophilic acid
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Sodium-Potassium-Exchanging ATPase